C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) A61K 31/435 (2006.01)
Patent
CA 2465416
Amine salts of 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-yl)- propyl]imidazolidin-1-yl}-3-(6-methoxy-pyridin-3-yl)propionic acid are potent antagonists of the integrin .alpha.v.szlig.3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts.
L'invention concerne des sels aminés d'acide 3-{2-oxo-3-[3-(5,6,7,8-tétrahydro[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3-(6-méthoxy-pyridin-3-yl)propionique constituant des antagonistes puissants du récepteur de l'intégrine .alpha.v.beta.3, et s'avérant utiles pour la prévention et/ou le traitement de l'ostéoporose et de la resténose vasculaire, ainsi que des troubles associés à une angiogénèse excessive, notamment une dégénération maculaire, une rétinopathie diabétique, une athérosclérose, une arthrite inflammatoire, un cancer, et une croissance tumorale métastatique. L'invention concerne également un procédé de préparation de nouveaux sels et de compositions pharmaceutiques contenant ces sels et des procédés d'utilisation de ces sels.
Wang Yaling
Wells Kenneth M.
Yasuda Nobuyoshi
Merck & Co. Inc.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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